Synthesis of Mefenamic Acid Containing N-Glycoconjugates and Their Evaluation as Human COX-2 Enzyme Inhibitor

Abstract

A series of d-glucose derived N-glycopeptides containing mefenamic acid have been synthesised and in vitro evaluation of all these molecules have been performed as COX-2 (human) enzyme inhibitor using Enzymes Immuno Assay kit. These studies were further supported by docking experiments on human COX-2 enzyme (PDB ID: 5IKR). All the compounds exhibited a fair amount of COX-2 enzyme inhibition during both the modes of study and tryptophan derivative showed the best activity. Acute toxicity (LD50) in rat has also been evaluated using General Unrestricted Structure-Activity Relationships (GUSAR) software, where acute oral toxicity for most of the molecules was found to be less than the pure mefenamic acid.